槲皮素对大鼠DRG神经元Nav1.8电流的作用及机制

发布时间：2018-02-09 08:32

本文关键词： 槲皮素背根神经节 Nav.通道电流全细胞膜片钳慢性内脏痛　出处：《中国药科大学学报》2015年01期 　论文类型：期刊论文

【摘要】：研究槲皮素(Que)对大鼠脊髓背根神经节(DRG)神经元Nav1.8通道电流(INav1.8)的作用。在急性分离的大鼠DRG神经元上,用全细胞膜片钳技术,观察Que干预INav1.8的剂量-反应关系以及Que影响的Nav1.8通道电压依赖的激活和失活特性。结果显示Que(10,30,100μmol/L)可浓度依赖地抑制DRG神经元INav1.8峰值,峰值抑制率分别为(15.32±3.43)%,(22.92±8.24)%和(47.29±11.42)%,半数抑制浓度(IC50)为121.38μmol/L,Hill系数为0.76;100μmol/L Que可使DRG神经元的Nav1.8通道激活曲线向去极化方向偏移了0.83 m V,失活曲线向超极化方向偏移了1.86 m V;且与干预前比,半数失活电压(V1/2)为-(40.23±0.25)m V,有显著性差异(P0.01)。说明Que可浓度依赖和电压依赖地抑制DRG神经元Nav1.8通道活性,进而降低痛觉信息的传递,改善慢性内脏痛。
[Abstract]:To study the effect of Quercetin on the Nav1.8 channel current of DRG neurons in rat spinal dorsal root ganglion (DRG). In acute isolated rat DRG neurons, whole-cell patch clamp technique was used. The dose-response relationship of Que intervention in INav1.8 and the activation and inactivation characteristics of Nav1.8 channel voltage dependence induced by Que were observed. The results showed that Quegnum 1030 渭 mol / L inhibited the INav1.8 peak of DRG neurons in a concentration-dependent manner. The peak inhibitory rates were 15.32 卤3.43% and 47.29 卤11.42%, respectively. IC50 was 121.38 渭 mol / L 路L ~ (-1) Que. The Nav1.8 channel activation curve of DRG neurons shifted to depolarization direction by 0.83 MV, and the inactivation curve shifted to hyperpolarization direction by 1.86 MV, compared with that before intervention. The half inactivated voltage (V 1 / 2) was -40. 23 卤0. 25mV, there was significant difference (P 0. 01). It indicated that Que could inhibit the Nav1.8 channel activity of DRG neurons in a concentration-and voltage-dependent manner, and then reduce the transmission of nociceptive information and improve chronic visceral pain.
【作者单位】：南京中医药大学附属医院江苏省中医院;南京中医药大学第一临床医学院;中国药科大学药理学研究室;香港浸会大学中医药学院;
【基金】：江苏省自然科学基金资助项目(No.BK20140959) 高等学校博士学科点专项科研基金资助项目(No.20133237110008)~~
【分类号】：R965

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